Elebsiran
Elebsiran (VIR-2218) is a siRNA that targets and degrades hepatitis B virus (HBV) and hepatitis D virus (HDV) RNA transcripts. Elebsiran leads to a significant decrease in HBV surface antigen (HBsAg) and a reduction in viral load. Elebsiran binds to the sialic acid-depleted glycoprotein receptor (ASGPR) on the surface of liver cells through the GalNAc ligand, achieving liver-targeted delivery and demonstrating improved liver safety. Elebsiran can be used for the study of chronic HBV/HDV infections.
The free form of the compound is prone to instability, it is advisable to consider the stable salt form (Elebsiran sodium) that retains the same biological activity.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 95.11%
- CAS 番号: 2648009-64-5
- 分子式: C485H618F9N158Na40O294P39S6
- 分子量:14976.67
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保管条件:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
生物活性
製品説明
体外実験
Elebsiran (0.1 pM-100 nM) effectively reduces HBsAg and the infectivity of HDV, and when combined with Tobevibart (HY-P990015) for treatment, it shows an additive effect[1].
Elebsiran exhibits comparable antiviral activity to ALN-HBV in HepG2.2.15 cells but its cytotoxicity is significantly reduced[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
体内実験
Elebsiran (12-100 mg/kg, s.c., 5 doses on Days 0, 21, 28, 35, and 42) does not cause a significant increase in ALT in all dosage groups and demonstrates high liver safety in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HBV/HDV-coinfected liver-chimeric model established in liver-chimeric mice[1]
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Dosage:9 mg/kg alone or with 15 mg/kg muHBC34 (the murinized version of Tobevibart)
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Administration:Subcutaneous injection (s.c.), single dose
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Result:Significant decreased of 0.6 log for HBsAg, 0.5 log for HBV DNA and 0.7 log for HDV RNA compared to the vehicle control on day 14 post-treatment.
Led to the strongest reductions in HBsAg, HBV DNA and HDV RNA levels relative to the vehicle group with muHBC34.
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Animal Model:Chimeric mouse model established male PXB mice at 12 to 18 weeks[3]
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Dosage:12 mg/kg, 36 mg/kg, and 100 mg/kg
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Administration:Subcutaneous injection (s.c.), on Days 0, 21, 28, 35, and 42
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Result:Observed a clear dose-dependent increase in hALT1 levels, whereas no relationship between hALT1 and dose level.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2648009-64-5
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性状 Solid
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分子量 14976.67
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分子式 C485H618F9N158Na40O294P39S6
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Color White to off-white
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SMILES
[Elebsiran]
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別名
VIR-2218
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
純度とドキュメンテーション
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データシート (270 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Zhou J, et al. Therapy with murinized tobevibart and elebsiran is efficacious in a liver-chimeric mouse model of HDV infection. JHEP Rep. 2025 Mar 22;7(6):101400. [Content Brief]
[2]. Gupta SV, et al. Clinical and Preclinical Single-Dose Pharmacokinetics of VIR-2218, an RNAi Therapeutic Targeting HBV Infection. Drugs R D. 2021 Dec;21(4):455-465. [Content Brief]
[3]. Ji Y, et al. The Impact of Hepatitis B Surface Antigen Reduction via Small Interfering RNA Treatment on Natural and Vaccine (BRII-179)-Induced Hepatitis B Virus-Specific Humoral and Cellular Immune Responses. Gastroenterology. 2025 Jul;169(1):136-149. [Content Brief]
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)